
Capsaicin bestows spiciness by activating TRPV1 channel with exquisite potency and selectivity. Although a capsaicin-bound channel structure was previously resolved by cryo-EM at 4.2- to 4.5-Å resolution, capsaicin was registered as a small electron density, reflecting neither its chemical structure nor specific ligand-channel interactions--important details required for mechanistic understanding. We obtained the missing atomic-level details by iterative computation and confirmed them by systematic site-specific functional tests. We observed that the bound capsaicin takes a 'tail-up, head-down' configuration. The vanillyl and amide groups form specific interactions to anchor its bound position, while the aliphatic tail may sample a range of conformations, making it invisible in cryo-EM images. Capsaicin stabilizes TRPV1's open state by 'pull-and-contact' interactions between the vanillyl group and the S4-S5 linker. Our study provides a structural mechanism for the agonistic function of capsaicin and its analogs, and demonstrates an effective approach to obtain atomic-level information from cryo-EM structures.
Biochemistry & Molecular Biology, Patch-Clamp Techniques, Recombinant Fusion Proteins, Molecular Sequence Data, Sequence Homology, TRPV Cation Channels, Gene Expression, Article, Medicinal and Biomolecular Chemistry, Mice, Species Specificity, Bacterial Proteins, Animals, Humans, Point Mutation, Amino Acid Sequence, Dental/Oral and Craniofacial Disease, Pain Research, Cryoelectron Microscopy, Rats, Molecular Docking Simulation, Amino Acid, Kinetics, Luminescent Proteins, HEK293 Cells, Biochemistry and Cell Biology, Rabbits, Capsaicin, Sequence Alignment, Chickens, Ion Channel Gating, Protein Binding
Biochemistry & Molecular Biology, Patch-Clamp Techniques, Recombinant Fusion Proteins, Molecular Sequence Data, Sequence Homology, TRPV Cation Channels, Gene Expression, Article, Medicinal and Biomolecular Chemistry, Mice, Species Specificity, Bacterial Proteins, Animals, Humans, Point Mutation, Amino Acid Sequence, Dental/Oral and Craniofacial Disease, Pain Research, Cryoelectron Microscopy, Rats, Molecular Docking Simulation, Amino Acid, Kinetics, Luminescent Proteins, HEK293 Cells, Biochemistry and Cell Biology, Rabbits, Capsaicin, Sequence Alignment, Chickens, Ion Channel Gating, Protein Binding
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